SB216763
SB216763 是一种有效的，选择性GSK-3α抑制剂，IC50为34.3 nM；对GSK-3β具有同样的抑制作用。SB216763 可激活自噬。
SB216763 Chemical Structure
CAS: 280744-09-4
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SB216763相关产品
相关信号通路图
GSK-3抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HepG2 | Function assay | 34 uM | 12 hrs | Inhibition of GSK3beta in human HepG2 cells assessed as decrease in ratio of phosphorylated GS/GS at 34 uM after 12 hrs by Western blot analysis | 25467150 |
| 3T3L1 | Function assay | 34 uM | 12 hrs | Increase in glucose incorporation in mouse 3T3L1 cells at 34 uM after 12 hrs by glucose assay | 25467150 |
| HepG2 | Function assay | 34 uM | 12 hrs | Increase in glucose incorporation in human HepG2 cells at 34 uM after 12 hrs by glucose assay | 25467150 |
| ReNcell VM | Antiproliferative assay | 3 uM | 72 hrs | Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs | 20708937 |
| Sf9 | Function assay | 30 min | Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting, IC50=0.03388μM | SANGER | |
| MIAPaCa2 | Growth inhibition assay | 72 hrs | Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=25μM | 19338355 | |
| ST14A | Function assay | 6 hrs | Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis | 20708937 | |
| human SF539 cell | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM | SANGER | ||
| human NCI-SNU-1 cell | Growth inhibition assay | Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=21.5558 μM | SANGER | ||
| human BxPC-3 cell | Growth inhibition assay | Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 μM | SANGER | ||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=21.1879 μM | SANGER | ||
| human U-266 cell | Growth inhibition assay | Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 μM | SANGER | ||
| human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=19.4549 μM | SANGER | ||
| human MKN45 cell | Growth inhibition assay | Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 μM | SANGER | ||
| human BHT-101 cell | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=17.6099 μM | SANGER | ||
| human IGROV-1 cell | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 μM | SANGER | ||
| human YH-13 cell | Growth inhibition assay | Inhibition of human YH-13 cell growth in a cell viability assay, IC50=16.6865 μM | SANGER | ||
| human S-117 cell | Growth inhibition assay | Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 μM | SANGER | ||
| human QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=15.6394 μM | SANGER | ||
| human D-566MG cell | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 μM | SANGER | ||
| human A2058 cell | Growth inhibition assay | Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM | SANGER | ||
| human LoVo cell | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 μM | SANGER | ||
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=13.2427 μM | SANGER | ||
| human RPMI-7951 cell | Growth inhibition assay | Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 μM | SANGER | ||
| human NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.7264 μM | SANGER | ||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 μM | SANGER | ||
| human NB5 cell | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay, IC50=11.2157 μM | SANGER | ||
| human ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 μM | SANGER | ||
| human G-361 cell | Growth inhibition assay | Inhibition of human G-361 cell growth in a cell viability assay, IC50=10.1798 μM | SANGER | ||
| human ESS-1 cell | Growth inhibition assay | Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 μM | SANGER | ||
| human SK-OV-3 cell | Growth inhibition assay | Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.1002 μM | SANGER | ||
| human IST-SL1 cell | Growth inhibition assay | Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 μM | SANGER | ||
| human NCI-H1993 cell | Growth inhibition assay | Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=8.36534 μM | SANGER | ||
| human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 μM | SANGER | ||
| human HMV-II cell | Growth inhibition assay | Inhibition of human HMV-II cell growth in a cell viability assay, IC50=7.67607 μM | SANGER | ||
| human GAMG cell | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 μM | SANGER | ||
| human LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.42874 μM | SANGER | ||
| human BT-549 cell | Growth inhibition assay | Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 μM | SANGER | ||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=2.69685 μM | SANGER | ||
| human K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 μM | SANGER | ||
| human JAR cell | Growth inhibition assay | Inhibition of human JAR cell growth in a cell viability assay, IC50=1.21044 μM | SANGER | ||
| human HOP-62 cell | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 μM | SANGER | ||
| human NCI-H1770 cell | Growth inhibition assay | Inhibition of human NCI-H1770 cell growth in a cell viability assay. IC50=0.29392 μM | SANGER | ||
| human HDLM-2 cell | Growth inhibition assay | Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 μM | SANGER | ||
| neural precursor cells | Function assay | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 17417631 | ||
| HEK293 | Function assay | Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2μM | 12941331 | ||
| HEK293 | Function assay | Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells, EC50=0.2μM | 15149684 | ||
| human VA-ES-BJ cell | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=22.5763 μM | SANGER | ||
| human HuO-3N1 cell | Growth inhibition assay | Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=22.6151 μM | SANGER | ||
| human EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50=22.6689 μM | SANGER | ||
| human T98G cell | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50=23.3009 μM | SANGER | ||
| human SW1783 cell | Growth inhibition assay | Inhibition of human SW1783 cell growth in a cell viability assay, IC50=23.5243 μM | SANGER | ||
| human NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=23.8512 μM | SANGER | ||
| human KOSC-2 cell | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=24.1292 μM | SANGER | ||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6067 μM | SANGER | ||
| human NCI-H28 cell | Growth inhibition assay | Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=25.2104 μM | SANGER | ||
| human 5637 cell | Growth inhibition assay | Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM | SANGER | ||
| human NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=26.1764 μM | SANGER | ||
| human HT-29 cell | Growth inhibition assay | Inhibition of human HT-29 cell growth in a cell viability assay, IC50=27.1752 μM | SANGER | ||
| human PFSK-1 cell | Growth inhibition assay | Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=27.593 μM | SANGER | ||
| human UACC-257 cell | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=27.743 μM | SANGER | ||
| human D-423MG cell | Growth inhibition assay | Inhibition of human D-423MG cell growth in a cell viability assay, IC50=27.9106 μM | SANGER | ||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=28.4059 μM | SANGER | ||
| human DEL cell | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay, IC50=29.0474 μM | SANGER | ||
| human LS-513 cell | Growth inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50=30.1334 μM | SANGER | ||
| human NBsusSR cell | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=30.5678 μM | SANGER | ||
| human BV-173 cell | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50=30.7649 μM | SANGER | ||
| human A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM | SANGER | ||
| human LU-134-A cell | Growth inhibition assay | Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=31.0238 μM | SANGER | ||
| human ES3 cell | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50=31.3376 μM | SANGER | ||
| human NY cell | Growth inhibition assay | Inhibition of human NY cell growth in a cell viability assay, IC50=32.2965 μM | SANGER | ||
| human NCI-H1975 cell | Growth inhibition assay | Inhibition of human NCI-H1975 cell growth in a cell viability assay, IC50=32.3582 μM | SANGER | ||
| human A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=34.2059 μM | SANGER | ||
| human SK-MEL-24 cell | Growth inhibition assay | Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=34.2523 μM | SANGER | ||
| human SW1088 cell | Growth inhibition assay | Inhibition of human SW1088 cell growth in a cell viability assay, IC50=34.3452 μM | SANGER | ||
| human SK-MEL-1 cell | Growth inhibition assay | Inhibition of human SK-MEL-1 cell growth in a cell viability, IC50=34.714 μM | SANGER | ||
| human MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=36.1467 μM | SANGER | ||
| human T47D cell | Growth inhibition assay | Inhibition of human T47D cell growth in a cell viability assay, IC50=37.1647 μM | SANGER | ||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=37.3608 μM | SANGER | ||
| human MKN7 cell | Growth inhibition assay | Inhibition of human MKN7 cell growth in a cell viability assay, IC50=38.0909 μM | SANGER | ||
| human CAL-72 cell | Growth inhibition assay | Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=38.1178 μM | SANGER | ||
| human AGS cell | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50=38.2039 μM | SANGER | ||
| human BE-13 cell | Growth inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50=38.7783 μM | SANGER | ||
| human Calu-6 cell | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=39.6964 μM | SANGER | ||
| human CAL-27 cell | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.0054 μM | SANGER | ||
| human BB49-HNC cell | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=44.0278 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | SB216763 是一种有效的，选择性GSK-3α抑制剂，IC50为34.3 nM；对GSK-3β具有同样的抑制作用。SB216763 可激活自噬。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 除了抑制GSK-3α,SB 216763也同样有效作用于 GSK-3β，按10 μM 处理，抑制达96%， 作用于24 种其他蛋白激酶包括 PKBα 和PDK1时具有最小活性，IC50>10 μM。SB-216763作用于人肝脏细胞，刺激糖原合成，EC50为3.6 μM, 且作用于HEK293 细胞，诱导β-catenin-LEF/TCF相关报告基因的转录，这种作用存在剂量依赖性，按 5 μM处理，诱导达到最大值，增大2.5倍。[1]与剂量依赖性显著抑制GSK-3 活性一致，SB 216763 保护小脑颗粒神经元免受 LY-294002或钾丧失而诱导的细胞凋亡，这种作用具有浓度依赖性，3 μM 时保护神经达到最高值，与10 mM LiCl作用效果形成对比。3 μM SB 216763完全抑制 LY-294002诱导的 鸡背根神经节感觉神经元死亡。5 μM SB 216763 作用于HEK293细胞，显著抑制小脑颗粒神经元中GSK-3依赖的神经元特异性微管相关蛋白的磷酸化，且提高β-catenin细胞质水平，与Wnt调节的 GSK-3抑制效果差不多。[2] 25-50 μM SB 216763作用于前列腺癌细胞系，包括BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC, 降低细胞活力，这种作用存在剂量依赖性，且显著促进凋亡，处理72小时,凋亡达50%,而对HMEC或WI38细胞系没有作用效果。[3] | |||
|---|---|---|---|---|
| 激酶实验 | GSK-3 活性检测 | |||
| 在不同浓度SB 216763存在时,在含1 nM 人GSK-3α, 50 mM MOPS pH 7.0,0.2 mM EDTA, 10 mM Mg(Ac)2,7.5 mM β-巯基乙醇,5% (w/v)甘油,0.01% (w/v) Tween-20, 10% (v/v) DMSO, 及28 μM GS-2 肽底物的反应混合物中，测量GSK-3激酶活性。GS-2肽序列对应GSK-3使糖原合酶磷酸的地区。加入0.34 μCi [33P]γ-ATP开始实验。全部ATP浓度为 10 μM。实验在室温下进行30分钟后，加入含21 mM ATP的1/3实验体积为2.5%(v/v) H3PO4，终止反应。样本在P30磷酸纤维垫上展开，然后在0.5% (v/v) H3PO4中冲洗6次。过滤垫密封到Wallac betaplate闪烁液的样品袋中。在 Wallac microbeta闪烁计数器中计算测定33P 渗透到底物肽中的量。 | ||||
| 细胞实验 | 细胞系 | BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC | ||
| 浓度 | 溶于DMSO, 终浓度为~50 μM | |||
| 孵育时间 | 24, 48, 和72小时 | |||
| 方法 | 使用不同浓度SB 216763处理细胞 24,48和 72小时。通过MTS检测测量相对细胞活力。使用 Hoechst染色而测定凋亡细胞。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pGSK-3β / GSK-3β / E2F1 / β-catenin c-Myb |
|
28042322 | |
| Growth inhibition assay | Cell viability |
|
24779365 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | SB 216763 按20 mg/kg 剂量处理患Bleomycin (BLM)诱导肺部炎症和纤维化的小鼠，通过显著抑制炎症细胞因子MCP-1和TNF-α的产量，显著抑制肺部炎症和纤维化，且显著提高BLM处理小鼠的寿命。SB 216763 处理，通过抑制肺泡上皮细胞损伤，而显著降低 BLM诱导的肺泡。[4] | |
|---|---|---|
| 动物实验 | Animal Models | 患Bleomycin (BLM)诱导的肺部炎症和纤维化的C57BL/6N小鼠 |
| Dosages | 20 mg/kg | |
| Administration | 静脉注射 | |
化学信息&溶解度
| 分子量 | 371.22 | 分子式 | C19H12N2O2Cl2 |
| CAS号 | 280744-09-4 | SDF | Download SB216763 SDF |
| Smiles | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 23 mg/mL ( (61.95 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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